Additional Hetero Ring Attached Directly Or Indirectly By Nonionic Bonding To The Seven-membered Hetero Ring Patents (Class 514/212.08)
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Publication number: 20110034439Abstract: To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed.Type: ApplicationFiled: April 9, 2009Publication date: February 10, 2011Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshimitsu Suda, Kosuke Egami, Hidenori Fujita
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Publication number: 20110009387Abstract: The present invention relates e.g., to methods for predicting cellular sensitivity to farnesyl protein transferase inhibitors, such as lonafarnib; manumycin A; FTI-276; L-744832; BMS-214662; tipifarnib; BMS-316810K. The methods involve determining if malignant cells exhibit increased expression. of phosphorylated histone H2Ax following contact of one or more of said cells with said inhibitor.Type: ApplicationFiled: June 11, 2008Publication date: January 13, 2011Inventor: Andrea Dawn Basso-Porcaro
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Publication number: 20110003794Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: August 30, 2010Publication date: January 6, 2011Inventor: Brian A Johns
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Publication number: 20110003788Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: ApplicationFiled: February 25, 2009Publication date: January 6, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Publication number: 20100323994Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Brian E. Fink, Soong-Hoon Kim, Yufen Zhao, Ping Chen, Wayne Vaccaro, Litai Zhang, Ashvinikumar V. Gaval, Dharmpal S. Dodd, Libing Chen
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Publication number: 20100298295Abstract: The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or anaplastic lymphoma kinase (ALK).Type: ApplicationFiled: August 27, 2008Publication date: November 25, 2010Applicant: IRM LLCInventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Badry Bursulaya, Christian Cho-Hua Lee, Nathanael S. Gray
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Publication number: 20100286122Abstract: An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1?-carbonyldiimidazole (“CDI”) as carbonyl source; an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide; efficient syntheses for the preparation of intermediates (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamiType: ApplicationFiled: April 6, 2007Publication date: November 11, 2010Inventor: Kevin Belyk
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Publication number: 20100279986Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Inventors: Yue-Mei ZHANG, Bangping Xiang, Shyh-Ming Yang, Kenneth Rhodes, Robert Scannevin, Paul Jackson, Davraj Chakravarty, Xiaodong Fan, Lawrence J. Wilson, Prabha Karnachi
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Publication number: 20100280006Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: May 8, 2009Publication date: November 4, 2010Inventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Patent number: 7820647Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N—Rb—, —O— or —S—; Ra may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb—, o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: GrantFiled: May 17, 2005Date of Patent: October 26, 2010Assignee: BASF AktiengesellschaftInventors: Anja Schwögler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Müller, Thomas Grote, Wassilios Grammenos, Udo Hünger, Carsten Blettner, Peter Schäfer, Oliver Wagner, Reinhard Stierl, Ulrich Schöfl, Siegfried Strathmann, Maria Scherer
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Publication number: 20100256113Abstract: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.Type: ApplicationFiled: September 25, 2008Publication date: October 7, 2010Applicant: Astellas Pharma Inc.Inventors: Kenichi Onda, Kenichiro Imamura, Fumie Sato, Hiroyuki Moritomo, Yasuharu Urano, Yuki Sawada, Naoki Ishibashi, Keita Nakanishi, Kazuhiro Yokoyama, Shigetada Furukawa, Kazuhiro Momose
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Publication number: 20100249102Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: April 6, 2010Publication date: September 30, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur Taveras
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Publication number: 20100222320Abstract: Compounds of formula I: Selectively attenuate production of A?(1-42) and hence find use in treatment or prevention of diseases associated with deposition of A? in the brain, in particular Alzheimer's disease.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Inventors: Christian Fischer, Ben Munoz, Susan Zultanski, Joey Methot, Hua Zhou, W. Colby Brown
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Publication number: 20100221259Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
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Publication number: 20100222326Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 24, 2008Publication date: September 2, 2010Applicant: UCB PHARMA, S.A.Inventors: Benoit Kenda, Laurent Turet, Yannick Quesnel, Philippe Michel, Ali Ates
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Publication number: 20100203039Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: April 16, 2010Publication date: August 12, 2010Inventor: Chu-Biao Xue
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Publication number: 20100190774Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: ApplicationFiled: April 8, 2010Publication date: July 29, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
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Publication number: 20100179127Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Philipp Floersheim, Wolfgang Froestl, Sebastien Guery, Kiemens Kaupmann, Manuel Koller
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Patent number: 7723324Abstract: Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed.Type: GrantFiled: October 28, 2004Date of Patent: May 25, 2010Assignee: Sepracor, Inc.Inventors: Q. Kevin Fang, Paul Grover, Thomas P. Jerussi
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Publication number: 20100125062Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 16, 2009Publication date: May 20, 2010Applicant: AMEN INC.Inventors: Jennifer R. Allen, Kaustav Biswas, Frank Chavez, Jr., Ning Chen, Frenel Fils Demorin, James R. Falsey, Mike Frohn, Paul Harrington, Dan Horne, Essa Hu, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Tom Nguyen, Alex Pickrell, Andreas Reichelt, Shannon Rumfelt, Rob Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20100119510Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: January 22, 2010Publication date: May 13, 2010Applicant: Bristol-Myers Squibb CompanyInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Patent number: 7662956Abstract: The present application relates to novel tetrahydrobenzo[d]azepin-2-one derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidaemias, arteriosclerosis, restenosis and ischaemias.Type: GrantFiled: February 1, 2005Date of Patent: February 16, 2010Assignee: Bayer Shering Pharma AGInventors: Nils Griebenow, Timo Flessner, Michael Härter, Martin Raabe, Anja Buchmüller, Hilmar Bischoff, Peter Ellinghaus, Peter Kolkhof
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Patent number: 7659264Abstract: The present invention is directed to compounds of Formula I: Formula I: I and Formula II: (where variables R1, R2, R3, R4, A, B, J, Q, T, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 5, 2005Date of Patent: February 9, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, James Z. Deng, Craig Potteiger, Theresa M. Williams
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Publication number: 20100029615Abstract: The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, A, X, n, and are as defined herein. Such novel benzamidazole derivatives are useful in trv treatment of abnormal cell growth, such as cancer, in mammals. This invention ate relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing sue compounds.Type: ApplicationFiled: December 5, 2007Publication date: February 4, 2010Inventors: Michael John Munchhof, Lawrence Alan Reiter, Andrei Shavnya, Christopher Scott Jones, Qifang Li, Robert Gerald Linde ll
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Publication number: 20100009967Abstract: A solid dosage pharmaceutical formulation comprising as an active ingredient the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide (telcagepant), arginine, and a pharmaceutically acceptable surfactant. The invention is also directed to an amorphous form of the potassium salt of telcagepant.Type: ApplicationFiled: June 29, 2009Publication date: January 14, 2010Inventors: Majid Mahjour, Dina Zhang, Aaron J. Moment
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Publication number: 20090264404Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: August 31, 2006Publication date: October 22, 2009Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20090258857Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: June 13, 2007Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20090215746Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: ApplicationFiled: October 31, 2008Publication date: August 27, 2009Applicant: Takeda Pharmaceuticals Company LimitedInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Patent number: 7569562Abstract: The invention provides N-substituted heterocyclic-sulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, Z and n are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).Type: GrantFiled: January 18, 2006Date of Patent: August 4, 2009Assignee: Elan Pharmaceuticals, Inc.Inventor: Martin Neitzel
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Publication number: 20090192139Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: April 3, 2009Publication date: July 30, 2009Inventors: Daniel V. Paone, Anthony W. Shaw
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Publication number: 20090176758Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: March 10, 2009Publication date: July 9, 2009Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Publication number: 20090149443Abstract: Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.Type: ApplicationFiled: March 27, 2007Publication date: June 11, 2009Inventors: Mark C. Munson, Kevin W. Hunt, Christopher T. Clark, Ganghyeok Kim, Laurence E. Burgess, James P. Rizzi
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Patent number: 7534784Abstract: The present invention is directed to compounds of Formula I: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: April 9, 2008Date of Patent: May 19, 2009Assignee: Merck + Co., Inc.Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
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Publication number: 20090093455Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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Publication number: 20090082337Abstract: Compositions for treating or controlling infections comprise a fluoroquinolone having Formulae I-VIII and have a pH in the range from about 3.5 to about 5.5 or from about 10.5 to about 12. Methods for treating or controlling such infection use such compositions. Such compositions and methods can deliver a higher amount of the fluoroquinolone to the affected site.Type: ApplicationFiled: September 8, 2008Publication date: March 26, 2009Inventors: Srini Venkastesh, Hongna Wang, Erning Xia, Matthew S. Jonasse
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Publication number: 20090075977Abstract: The present application describes deuterium-enriched MK-0974, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7501406Abstract: The invention relates to compounds of general formula wherein R1, R2, R3/R3?, R4/R4? and R5/R5? are as defined in the specification and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are ?-secretase inhibitors which can be useful in the treatment of Alzheimer's disease or common cancers including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.Type: GrantFiled: August 8, 2006Date of Patent: March 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Wolfgang Wostl
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Publication number: 20090054398Abstract: The invention provides a new method for treating disorders associated with activation of the Notch signal transduction pathway comprising administering an effective amount of a compound of Formula (I), in free form or in a pharmaceutically acceptable salt form or in the form of a pharmaceutically acceptable solvate of the compound or the salt, to a human or animal patient in need thereof.Type: ApplicationFiled: March 9, 2007Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Kevin Hudson, Naomi Laing, Paula Lewis
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Publication number: 20090029968Abstract: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.Type: ApplicationFiled: November 29, 2006Publication date: January 29, 2009Inventors: Bernard Christophe Barlaam, Robert Hugh Bradbury, Richard Ducray
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Publication number: 20080318928Abstract: The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as anticancer agents.Type: ApplicationFiled: August 19, 2008Publication date: December 25, 2008Applicant: AVENTIS PHARMA S.A.Inventors: Jidong ZHANG, Neerja Bhatnagar
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Publication number: 20080293692Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.Type: ApplicationFiled: December 4, 2007Publication date: November 27, 2008Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANYInventors: Richard E. Olson, Thomas P. Maduskuie, Lorin Andrew Thompson
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Publication number: 20080280857Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: April 9, 2008Publication date: November 13, 2008Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Theresa M. Williams
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Publication number: 20080275025Abstract: This invention relates to certain substituted lactam compounds, particularly caprolactam compounds, which are useful for the treatment of cancer.Type: ApplicationFiled: May 7, 2008Publication date: November 6, 2008Inventors: Kenneth Walter Bair, Frederick Ray Kinder, Richard William Versace
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Publication number: 20080176831Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N— or —S—; R1 may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: ApplicationFiled: May 17, 2005Publication date: July 24, 2008Applicant: BASF AktiengesellschaftInventors: Anja Schwogler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Muller, Thomas Grote, Wassilios Grammenos, Udo Hunger, Carsten Blettner, Peter Schafer, Oliver Wagner, Reinhard Stierl, Ulrich Schofl, Siegfried Strathmann, Maria Scherer
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080096867Abstract: Imidazo[1,2-a]pyridines of the formulae I and II: are disclosed. The compounds are useful to treat anxiety and insomnia. Pharmaceutical compositions and methods are also disclosed.Type: ApplicationFiled: October 28, 2004Publication date: April 24, 2008Applicant: Sepracor inc.Inventors: Q. Kevin Fang, Paul Grover, Thomas P. Jerussi
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Patent number: 7342022Abstract: The present invention relates to new compounds of formula I wherein R1, R2, R3, n, m are defined as in claim 1, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, especially in the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3Type: GrantFiled: December 18, 2002Date of Patent: March 11, 2008Assignee: AstraZeneca ABInventors: Stefan Berg, Ratan Bhat, Philip Edwards, Sven Hellberg
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Patent number: 7291612Abstract: The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions which may benefit from immunomodulation, including rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28.Type: GrantFiled: May 30, 2006Date of Patent: November 6, 2007Assignee: Active Biotech A.B.Inventors: Ian Richard Matthews, Thomas Stephen Coutler, Chiara Ghiron, Chris James Brennan, Muhammed Kamal Uddin, Lars Olof Goran Pettersson, Dorthe da Graca Thrige, Philip Huxley
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Patent number: 7268134Abstract: The present invention relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory response in endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating HSPGs such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as restenosis and atherosclerosis.Type: GrantFiled: September 27, 2004Date of Patent: September 11, 2007Assignee: Reddy US Therapeutics, Inc.Inventors: Richard T. Timmer, Christopher W. Alexander, Sivaram Pillarisetti, Uday Saxena, Koteswar Rao Yeleswarapu, Manojit Pal, Jangalgar Tirupathy Reddy, Velagala Venkata Rama Murali Krishna Reddy, Sesha Sridevi Alluri, Potlapally Rajender Kumar, Gaddam Om Reddy